Constitutively active phosphatidylinositol 3-kinase and uses thereof

US6300111A · kind A · utility

Assignee

• The Regents of the University of California · US

Inventors

• Anke Klippel · San Francisco, US
• Lewis T. Williams · San Francisco, US

Key dates

• Filing date: Mar 10, 1999
• Grant date: Oct 9, 2001
• Expiry date: Mar 10, 2019

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S435/975
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention provides a method of producing a constitutively active phosphatidylinositol 3-kinase (PI 3-kinase) comprising the catalytic p110 subunit covalently attached at the N-terminus to the iSH2 region of the regulatory subunit, p85. The invention discloses one form of the constitutively active kinase, p110*, which functions independently of growth factor stimulation. Expression vectors encoding a constitutively active PI 3-kinase and cells containing such expression vectors are provided. The invention also provides methods of using the constitutively active phosphatidylinositol 3-kinase to generate phosphoinositides, to identify cellular target proteins and associating molecules of PI 3-kinase, to screen for inhibitors of PI 3-kinase activity and to treat certain diseases, in particular, proliferative diseases. Kits comprising the constitutively active kinase are also provided.